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Solid phase polypeptide synthesis preparation method for leuprorelin

A technology of solid-phase peptide synthesis and leuprolide, which is applied in the preparation method of peptides, chemical instruments and methods, peptides, etc., can solve the problems of three wastes pollution, high production cost, and environmental pollution.

Active Publication Date: 2012-03-21
SHANGHAI SOHO YIMING PHARMA
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Problems solved by technology

[0006] There are certain defects in the current methods. Trifluoroacetic acid must be used for each round of decapping, so the peptide yield is low, resulting in high production costs; there are many wastes, and trifluoroacetic acid is used for purification, which pollutes the environment. The rate is generally below 25%
Therefore current methods limit the large-scale production and use of leuprolide acetate

Method used

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Examples

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Embodiment 1

[0091] The list of raw materials adopted in the embodiment and the foregoing process is as follows:

[0092] no product name manufacturer 1 Wang Resin Tianjin Hecheng Technology Co., Ltd. 2 Fmoc-Pro-OH Sichuan Sangao Biochemical Co., Ltd. 3 Fmoc-Arg(Pbf)-OH Sichuan Sangao Biochemical Co., Ltd. 4 Fmoc-Leu-OH Sichuan Sangao Biochemical Co., Ltd. 5 Fmoc-D-Leu-OH Sichuan Sangao Biochemical Co., Ltd. 6 Fmoc-Tyr(tBu)-OH Sichuan Sangao Biochemical Co., Ltd. 7 Fmoc-Ser(tBu)-OH Sichuan Sangao Biochemical Co., Ltd. 8 Fmoc-Trp-OH Sichuan Sangao Biochemical Co., Ltd. 9 Fmoc-His(Trt)-OH Sichuan Sangao Biochemical Co., Ltd.

[0093] 10 p-Glu-OH Sichuan Sangao Biochemical Co., Ltd. 11 1-Hydroxybenzotriazole (HOBt) Sichuan Sangao Biochemical Co., Ltd. 12 TBTU Sichuan Sangao Biochemical Co., Ltd. 13 Trifluoroacetic acid (TFA) Merck 14 N-Methylmorpholine (NMM) Merc...

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PUM

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Abstract

The invention discloses a bright-ala-ruilin preparing method of solid-phase polypeptide, which comprises the following steps: adopting Wang resin or CTC resin as original material to connect amino with protective group to produce protective nonapeptide resin; removing Fmoc-protective group sequently; proceeding side-chain protective group synchronizingly and cutting peptide; connecting ethylaminethrough ethylamine-to-HOBT to produce crude product; proceeding separation and purifying through C18 (or C8) pillar to produce fine bright-ala-ruilin. The invention avoids the utility of poisonous agent, which improves the purifying, peptide connecting and obtaining rate.

Description

technical field [0001] The invention relates to a preparation method of leuprolide, in particular to a preparation method of solid-phase polypeptide synthesis of leuprolide. Background technique [0002] Leuprorelin, the Chinese name is Leuprorelin acetate, or other names for short: Leuprorelin, the English name is Leuprorelin, and the structural formula is pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro -NHC 2 h 5 , formula C 59 h 84 N 16 o 12 .C 2 h 4 o 2 , the molecular weight is 1269.48. [0003] Leuprolide is clinically used to treat related hormone disorders, including advanced prostate cancer, endometriosis, central precocious puberty, etc. [0004] Leuprolide acetate is a gonadotropin-releasing hormone analog, which mainly acts on the anterior lobe of the pituitary gland. In the early stage of high-dose application, it can cause a transient increase in the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). It leads to decreased sensitivity ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K1/04
CPCY02P20/55
Inventor 周达明
Owner SHANGHAI SOHO YIMING PHARMA
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